1ta6

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[[Image:1ta6.gif|left|200px]]
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{{STRUCTURE_1ta6| PDB=1ta6 | SCENE= }}
{{STRUCTURE_1ta6| PDB=1ta6 | SCENE= }}
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'''Crystal structure of thrombin in complex with compound 14b'''
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===Crystal structure of thrombin in complex with compound 14b===
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==Overview==
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As part of an ongoing effort to prepare therapeutically useful orally active thrombin inhibitors, we have synthesized a series of compounds that utilize nonbasic groups in the P1 position. The work is based on our previously reported lead structure, compound 1, which was discovered via a resin-based approach to varying P1. By minimizing the size and lipophilicity of the P3 group and by incorporating hydrogen-bonding groups on the N-terminus or on the 2-position of the P1 aromatic ring, we have prepared a number of derivatives in this series that exhibit subnanomolar enzyme potency combined with good in vivo antithrombotic and bioavailability profiles. The oxyacetic amide compound 14b exhibited the best overall profile of in vitro and in vivo activity, and crystallographic studies indicate a unique mode of binding in the thrombin active site.
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(as it appears on PubMed at http://www.pubmed.gov), where 9703466 is the PubMed ID number.
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{{ABSTRACT_PUBMED_9703466}}
==About this Structure==
==About this Structure==
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[[Category: Yan, Y.]]
[[Category: Yan, Y.]]
[[Category: Thrombin inhibitor complex]]
[[Category: Thrombin inhibitor complex]]
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Revision as of 23:27, 27 July 2008

Image:1ta6.png

Template:STRUCTURE 1ta6

Crystal structure of thrombin in complex with compound 14b

Template:ABSTRACT PUBMED 9703466

About this Structure

1TA6 is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

Design and synthesis of a series of potent and orally bioavailable noncovalent thrombin inhibitors that utilize nonbasic groups in the P1 position., Tucker TJ, Brady SF, Lumma WC, Lewis SD, Gardell SJ, Naylor-Olsen AM, Yan Y, Sisko JT, Stauffer KJ, Lucas BJ, Lynch JJ, Cook JJ, Stranieri MT, Holahan MA, Lyle EA, Baskin EP, Chen IW, Dancheck KB, Krueger JA, Cooper CM, Vacca JP, J Med Chem. 1998 Aug 13;41(17):3210-9. PMID:9703466

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